Multidrug-resistant (MDR) pathogens represent a growing threat to human health, with many infectious diseases effectively regressing toward the pre-antibiotic era, exemplified by the dramatic rise of community-acquired methicillin-resistant Staphylococcus aureus (MRSA) infections. Methicillin-resistant Staphylococcus aureus (MRSA) is one of the most prevalent multidrug-resistant pathogens worldwide, exhibiting increasing resistance to the latest antibiotic monotherapies used to treat these infections. The emergence of MRSA has virtually eliminated the use of β-lactams as therapeutic options against S. aureus. The recently developed β-lactam agent ceftaroline, which exhibits activity in treatment of MRSA infections, does so by binding to the allosteric site of PBP2a, triggering opening of the active site for inactivation by the drug; however, resistance to ceftaroline and other antibiotics used to treat MRSA, including linezolid, vancomycin, and daptomycin, has been reported. Thus, there is a need in the art for a new strategy to treat MDR pathogens and repurpose existing antibiotics.